NPS 2390

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

NPS 2390 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke. NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC₅₀ values equal to 5.2 and 82 nM, respectively). At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes. At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-selective antagonist, [³H]R214127, in rat cerebellum.

• Verwenden

  NPS 2390 is an inhibitor of CaSR (Calcium-sensing recpetor). NPS 2390 up-regulated anti-apoptotic protein Bcl-2 expression and down-regulated pro-apoptotic protein Bax.

• Verwenden

  Metabotropic glutamate receptors (mGluRs), mediate excitatory synaptic transmission in the central nervous system. Potent and selective antagonists of the type I mGluRs (mGluR1 and mGluR5) are of interest as novel therapeutics for the treatment of various CNS disorders, such as pain, epilepsy, and stroke. NPS 2390 is a first generation quinoxaline derivative that acts as a noncompetitive antagonist of mGluR1 and mGluR5 with IC50 values equal to 5.2 and 82 nM, respectively). At concentrations up to 30 μM, NPS 2390 does not affect mGluR2 or mGluR8 or a standard collection of 37 additional receptors, ion channels, and enzymes. At a dose of 10 mg/kg, NPS 2390 displaced the specifically bound mGlu1R-selective antagonist, [3H]R214127, in rat cerebellum.

• Lager

  Store at RT

NPS 2390 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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